Diflapolin
Based on 1 publication(s) in Google Scholar
Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s?of? 30 and 170?nM, respectively, and suppressed the activity of isolated sEH (IC50=20?nM).
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- Pureza: 99.33%
- No. CAS: 724453-98-9
- Fòrmula: C22H17Cl2N3O2S
- Peso molecular:458.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Diflapolin
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Actividad biológica
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD-1 mice (zymosan-induced peritonitis mouse model)[1]
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Dosage:1, 3 and 10 mg/kg
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Administration:I.p.; 30 min before zymosan injection
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Result:Induced a significant reduction of LTC4 and LTB4 peritoneal levels, starting from the dose of 1 mg/kg and comparable to the effect of MK886.
Chemical Information
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No. CAS 724453-98-9
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Appearance Solid
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Peso molecular 458.36
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Fòrmula C22H17Cl2N3O2S
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Color White to off-white
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SMILES
O=C(NC1=CC=C(Cl)C(Cl)=C1)NC2=CC=C(OCC3=NC4=CC=CC=C4S3)C=C2C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Pharm Sci
Encapsulation of the Anti-inflammatory Dual FLAP/sEH Inhibitor Diflapolin Improves the Efficiency in Human Whole Blood. [Abstract]2022 Jun;111(6):1843-1850. PMID: 34756868
Solvente y solubilidad
DMSO : 83.33 mg/mL (181.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.54 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1817 mL | 10.9085 mL | 21.8169 mL | 54.5423 mL |
| 5 mM | 0.4363 mL | 2.1817 mL | 4.3634 mL | 10.9085 mL | |
| 10 mM | 0.2182 mL | 1.0908 mL | 2.1817 mL | 5.4542 mL | |
| 15 mM | 0.1454 mL | 0.7272 mL | 1.4545 mL | 3.6362 mL | |
| 20 mM | 0.1091 mL | 0.5454 mL | 1.0908 mL | 2.7271 mL | |
| 25 mM | 0.0873 mL | 0.4363 mL | 0.8727 mL | 2.1817 mL | |
| 30 mM | 0.0727 mL | 0.3636 mL | 0.7272 mL | 1.8181 mL | |
| 40 mM | 0.0545 mL | 0.2727 mL | 0.5454 mL | 1.3636 mL | |
| 50 mM | 0.0436 mL | 0.2182 mL | 0.4363 mL | 1.0908 mL | |
| 60 mM | 0.0364 mL | 0.1818 mL | 0.3636 mL | 0.9090 mL | |
| 80 mM | 0.0273 mL | 0.1364 mL | 0.2727 mL | 0.6818 mL | |
| 100 mM | 0.0218 mL | 0.1091 mL | 0.2182 mL | 0.5454 mL |